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Description

A cell-permeable peptidomimetic that competes against MLL1 (Mixed Lineage Leukemia 1) minimum essential WIN (WDR5 INteracting) motif (-Ala3764-Arg-Ala3766-) for WDR5 (Trp-Asp Repeat Domain 5) binding (IC50/Ki = 2.5 nM/50 = 0.4 nM). Shown to reduce HoxA9 and Meis-1 mRNA expression (by 76% and 36%, respectively, after 96 h 50 µ,M MM-102 treatment) in myeloblasts derived from MLL1-AF9-transduced murine bone marrow cells and preferentially inhibit the growth of MLL1-AF4-harboring MV4,11 and MLL1-ENL-harboring KOPN8 leukemia cultures (GI50 in 7 days = 25 µ,M) via apoptosis induction (by >75% in 4 days in MV4:11 cultures, 50 µ,M MM-102), while exhibiting much reduced potency against BCR-ABL-dependent K562 cells (GI50 in 7 days = 84 µ,M, >90 live cells after 4-day 50 µ,M MM-102 treatment)., A cell-permeable peptidomimetic that prevents MLL1 (Mixed Lineage Leukemia 1) from complex assembling with WDR5 (Trp-Asp Repeat Domain 5), RbBP5 (Retinoblastoma Binding Protein 5), and ASH2L (Absent Small or Homeotic-2-Like) for enhanced H3K4 methyltransferase activity (IC50 = 0.4 nM). Shown to reduce HoxA9 and Meis-1 mRNA expression in myeloblasts derived from MLL1-AF9-transduced murine bone marrow cells (50 µ,M for 96 h) and preferentially inhibit the growth of MLL1-AF4-harboring MV4,11 and MLL1-ENL-harboring KOPN8 leukemia cultures (GI50 in 7 days = 25 µ,M) via apoptosis induction, while exhibiting much reduced potency against BCR-ABL-dependent K562 cells (GI50 in 7 days = 84 µ,M).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.